Therapeutic preparation comprising benzyl cinnamate and vitamin a



is disclosed which obtains better results.

Patented Apr. 8, 1952 UNITED {STATES PATENT OFFICE THERAPEUTIC PREPARATION' COMPRISING BENZY L GINNAMATE ANDTVITAMINA Jacob Jacobson, New York; N. NoDrawin'g. Application. Apri159,fi949.

. Serial N0. 86,592

i6 Claims. (Cl. 167-65) '1 This invention relates to therapeutic preparations adapted for subcutaneous or intramuscular injection containing vitamin A and a benzylic compound, such as benzyl alcohol or a benzyl ester. in a suitable vehicle.

The therapeutic properties of the benzyl ester of cinnamic acid have been extensively investigatedand the results are described in many publications among which may be mentioned the following: v

-Comptes Rendue Soc. 'de Dermatologie of :Eeb-

ruary .9, 1922--Articles by Darier and vJeanselme and Jacobson.

Bulletin et Mem. de la Soc. Med. des iHop., Reports of theSessions of October 28,.1925, March 25, 1927, and April 19, 1929.

La Presse Medicale, of March 13,.1929-Article by Gosset, Gutmann, and Iahel.

Paris Medical, of October 25, 1930-Article by .Levy-Solal, et a1.

Publication by Societe dOphtalmologie de Paris of February 1931--Article by Chevallereau :andSegal.

" 1933Article by Junes. 7

Bulletin of the Academy of .Medicine-Report of the Session-of July 18, 1933, volume 110, No. 28 oniRegression des keratites, etc.

- The preparation ordinarily employed consisted .,of.3.2 parts of benzyl cinnamate in solutionxin 100 parts of olive oil by volume.

In my prior Patent No. 2,081,934 a composition This composition is one in which the 3.2 parts of benzyl cinnamate is reduced and in part replaced by other ingredients which contribute one or both of the benzyl alcohol or cinnamic acid radicals. For instance, such a composition may be made from a mixture of about 20 grams of benzyl cinnamate, about 10 to cc. of benzyl alcohol and about 2 cc. of ethyl cinnamate. The mixture of these components is suspended in olive oil in approximately 3.2 parts of the mixture to about 100 parts of the olive oil suspension. The preparation is then placed in ampules and sterilized. The ordinary dose for a normal patient is from /2 to 1 cc., and the ordinary dose for a child is A cc. The preferred administration is by way of intramuscular and subcutaneous injection.

their location'in the organism.

The exact manner'in which thebenzyl cinnamate or benzyl alcohol and cinnamic acid acts is not exactly known, although its biological and physiological properties are manifest. Clinical experiments have demonstrated that the solution of the benzyl cinnamate or its chemical components favors the absorption or the elimination of chronic inflammatory lesions regardless of I have studied the vascular reaction which-is manifest upon the administration of benzyl cinnamate and from clinical "and experimental work on the corneal opacities, I have found that the action is characterized by a dilatation of the existing blood vessels, the opening of blocked blood vessels and the appearance of newly formed blood vessels.

The composition has beenparticularly effective in the treatment of certain forms of deafness, tinnitus and dizziness.

J. JacobsonzAnn. doto-laryngology, August, 1938, No. 8, pp. 775-781.

J.. Jacobson: Archives of Oto-La'ryngol, October, 1943, vol. 38, pp. 365- 368.

J. Jacobson: The Eye, Ear, Nose, and Throat Monthly, 232395-399, October 1944, and volume XXV, No. 11,- pp. 544-553, November 1946.

Samuel Kopetsky: Deafness, Tinnitus,Dizziness, Nelson and'So'n, 1948.

.In deafness, caused by a chronic inflammatory lesion of the middle ear, the benzyl cinnamate removes the obstacle created by chronic inflammation to the passage of the sound waves and the nerve endings are able to receive moreostimulation. Therefore, the hearing is improved.

Theiuseof the composition has been extended to the treatment of chronic salpingitis as reported in the following publication:

Morris I. Eisenstein, ,M. 'D., and .George J. Bendo, M..D.: Treatment of Chronic Salpingitis with Ben'zyl Cinnamate Ester (Jacobsons Solution), The American Journal of Surgery, vol. LXXIV, No. 2, August, 1947, pages 200-204.

In accordance with my invention I have now discovered that a composition containing benzyl cinnamate or its chemical components, as described in my patent and in the prior publications, to which vitamin A has been added, has markedly superior properties in achieving therapeutic properties.

The following examples are illustrative of the compositions made in accordance with my invention:

Example 1 An olive oil suspension containing 3.2 parts of benzyl cinnamate in parts by volume of the suspension has added to it vitamin A in the proportion of 10,000 units to each 1 cc. of the suspension.

Emample 2 An olive oil suspension of 2.5% of benzyl cinnamate has vitamin A added to it in the amount of 10,000 units of vitamin A for each 1 cc. of the suspension.

Example 3 A mixture of grams of benzyl cinnamate and 15 cc. of benzyl alcohol is suspended in olive oil in proportions approximately 3.2 parts of the mixture in 100 parts of the suspension. To this is added vitamin A in an amount of 10,000 units per 1 cc. of the suspension.

Example 4 An olive oil suspension of 1.5% of benzyl cinnamate and 2.0% of benzyl alcohol has added to it 10,000 units of vitamin A' per 1 cc. of the mixture.

Example 5 Olive oil containing 2.5% benzyl alcohol has added to it 10,000 units of vitamin A per 1 cc. of the mixture.

Any of the above examples may be modified by adding thereto of ethyl cinnamate.

The essential ingredients of the composition of my invention include vitamin A and benzyl alcohol or a benzyl ester yielding benzylalcohol such as benzyl cinnamate, or components furnishing these radicals, in an oil suspension. The benzyl cinnamate may be replaced in part or entirely by other compounds which furnish its chemical components and are therefore its equivalent. The amount of the benzylic compound or the chemical components which compose it may vary from 2% to 5% of the oil suspension, the optimum being from 2.5% to about 3.2%. The amount of vitamin A may vary from about 7,500 to 12,500 units per cc. of the oil suspension. The amount within this range is not thought to be critical.

The amounts of all of theingredients may be varied plus or minus The amounts are not critical, but the proportions expressed in the examples are the optimum concentrations containing various mixtures oi. benzyl cinnamate or benzyl alcohol and ethyl cinnamate, respond much better to the composition of my invention. The results are obtained in a shorter time; they are more permanent and the percentage of the refractory cases of tinnitus is markedly reduced. The composition of my invention is eflicacious in many refractory cases that do not respond to benzyl cinnamate, and are not affected at all by vitamin A alone.

The use of the preparation of my invention is applicable not only to the treatment of deafness but also to the various chronic inflammatory lesions, where the composition of my previous patent has been used, and with better results.

I claim:

1. A therapeutic composition comprising benzyl cinnamate in olive oil containing 2 to 5 parts of benzyl cinnamate per parts of the suspension and 7,500 to'12,500 units of vitamin A per cc. of the suspension.

2. A therapeutic composition comprising olive oil containing 2.5% to 3.2% benzyl cinnamate and 7,500 to 12,500 units of vitamin A per cc.

3. A therapeutic preparation, the essential ingredients of which are olive oil, about 3.2% benzyl cinnamate, and about 10,000 units of vitamin A per cc.

4. A therapeutic composition comprising olive oil and as essential therapeutic ingredients a mixture of benzyl cinnamate and benzyl alcohol and 7,500 to 12,500 units of vitamin A per cc.

5. A therapeutic composition comprising olive oil and as essential therapeutic ingredients a mixture of benzyl cinnamate, benzyl alcohol and ethyl cinnamate, and 7,500 to 12,500 units of vitamin A per cc.

6. A sterilized ampule-contained therapeutic preparation constituted of an olive oil suspension of a mixture containing benzyl cinnamic ester and benzyl alcohol in the approximate relation of 20 grams of the former in 15 cc. of the latter and with a total of suspended material approximating 3.2 parts in 100 parts of the suspension and about 7,500 to 12,500 units of vitamin A per cc. of the oil suspension.

' JACOB JACOBSON.

REFERENCES CITED The following references are of record in the file of this patent:

UNITED STATES PATENTS Number Name Date 2,081,934 Jacobson June 1, 1937 2,381,830 Lobel Aug. 7, 1945 OTHER REFERENCES Digest of Treatment, January 1950, pp. 100-101. 

1. A THERAPEUTIC COMPOSITION COMPRISING BENZYL CINNAMATE IN OLIVE CONTAINING 2 TO 5 PARTS OF BENZYL CINNAMATE PER 100 PARTS OF THE SUSPENSION AND 7,500 TO 12,500 UNITS OF VITAMIN A PER CC. OF THE SUSPENSION. 